Dofetilide

Catalog No.S1658 Synonyms: UK-68798

Dofetilide  Chemical Structure

Molecular Weight(MW): 441.56

Dofetilide is a selective potassium channel ((hERG)) blocker, used as a Class III antiarrhythmic drug.

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In DMSO USD 130 In stock
USD 97 In stock
USD 310 In stock
USD 670 In stock
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Biological Activity

Description Dofetilide is a selective potassium channel ((hERG)) blocker, used as a Class III antiarrhythmic drug.
Targets
Potassium channel [1]
In vitro

Dofetilide blocks HERG currents in excised macro patches of Xenopus oocytes. [1] Dofetilide (1 μM) reduces the amplitude of IKr to 61% of control currents in guinea pig cardiomyocytes, as measured by 200-ms test pulses and analysis of the deactivating tail currents of IKr. [2] Dofetilide increases apico-basal disparity of repolarization, due to a more marked increase of ERPs in the apex than in the base in the intact canine heart. [3]

In vivo Dofetilide (100 mg/kg, i.v.) does not suppress automaticity arrhythmias induced by two-stage coronary ligation and epinephrine or the coronary ligation and reperfusion arrhythmias, but suppresses the reentry arrhythmia induced by PES in dogs with old myocardial infarction (MI). Dofetilide also shows antiarrhythmic effect in some dogs with digitalis arrhythmia. Dofetilide increases QT interval and shows negative chronotropic effect like that of other class III drugs, but is different in antiarrhythmic profiles from those of other class III agents such as D-sotalol, E-4031, and MS-551 in that it does not prevent the occurrence of ventricular fibrillation (VF) immediately after coronary reperfusion and has some antiarrhythmic effects on digitalis arrhythmia. [4] Dofetilide causes increased resorptions and the same stage-dependent malformations in Sprague-Dawley rats. [5]

Protocol

Solubility (25°C)

In vitro DMSO 88 mg/mL warmed (199.29 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 441.56
Formula

C19H27N3O5S2

CAS No. 115256-11-6
Storage powder
Synonyms UK-68798

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02365532 Completed Long QT Syndrome Gilead Sciences February 2015 Phase 1
NCT02308748 Completed Drug-induced QT Prolongation|Pharmacokinetics|Pharmacodynamics Food and Drug Administration (FDA)|Spaulding Clinical Research LLC May 2014 Phase 1
NCT02439658 Recruiting Long QT Syndrome|Drug Toxicity Massachusetts General Hospital|VA Office of Research and Development|Beth Israel Deaconess Medical Center|Brigham and Womens Hospital January 2014 --
NCT01873950 Completed Drug-induced Surface ECG Changes Food and Drug Administration (FDA)|Spaulding Clinical Research LLC May 2013 Phase 1
NCT00408200 Completed Atrial Fibrillation University of Pennsylvania November 2006 --
NCT00392106 Suspended Atrial Fibrillation ProRhythm, Inc. April 2006 Phase 3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID